Fluorouracil

CLINICAL USE

Antineoplastic agent

DOSE IN NORMAL RENAL FUNCTION

IV infusion

: 15 mg/kg/day to a total dose of 12–15 gIV bolus: 12 mg/kg/day for 3 days, then 6 mg/kg on alternate days or 15 mg/kg once a weekMaintenance: 5–15 mg/kg once a week Intra-arterial infusion: 5–7.5 mg/kg by continuous 24-hour infusionOral: 15 mg/kg weekly; maximum 1 g in a dayOr consult relevant local chemotherapy protocol

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :130.1

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :10

%Excreted unchanged in urine &nbsp &nbsp : 15

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :0.25–0.5

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :16 minutes/Unchanged

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Some removal likely. Dose as in normal renal function

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Dialysed. Dose as in normal renal function

HDF/high flux &nbsp :Dialysed. Dose as in normal renal function

CAV/VVHD &nbsp &nbsp &nbsp:Dialysed. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anticoagulants: possibly enhances effect of coumarins

Antipsychotics: avoid concomitant use with clozapine, increased risk of agranulocytosisMetronidazole and cimetidine inhibit metabolism (increased toxicity)Temoporfin: increased skin photosensitivity with topical fluorouracil

ADMINISTRATION

Reconstition

Consult relevant local protocol

Route

IV infusion

intermittent or continuous, IV injection, intra-arterial, oral, topical

Rate of Administration

30–60 minutes, 4 hours or as a continuous infusion over 24 hours or consult relevant local protocol

Comments

–

OTHER INFORMATION

Use ideal body weight in patients showing obesity, ascites, and oedemaRoche recommends decreasing the initial dose by one-third to one-half in patients with impaired hepatic or renal functionDistributed throughout the body water, activated in target cells, most of dose (80%) is metabolised by the liver, 60–80% is excreted as respiratory CO2 and 2–3% by the biliary systemFollowing a single IV dose, approximately 15% is excreted unchanged in the urine.

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